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Ligand-Gated Ion Channels as Targets for Treatment and Management of Cancers.

Ligand-gated ion channels are an ionotropic receptor subtype characterized by the binding of an extracellular ligand, followed by the transient passage of ions through a transmembrane pore. Ligand-gated ion channels are commonly subcategorized into three superfamilies: purinoreceptors, glutamate receptors, and Cys-loop receptors. This classification is based on the differing topographical morphology of the receptors, which in turn confers functional differences. Ligand-gated ion channels have a diverse spatial and temporal expression which implicate them in key cellular processes. Given that t

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… Other clinical trials have focused on antagonizing the mGluR1 signaling pathway using riluzole with secondary outcomes being tumor shrinkage ( Barbara Ann Karmanos Cancer Institute, 2013 ; Rutgers, The State University of New Jersey, 2014 ). … A Phase I Trial of Riluzole in Combination With Radiation Therapy in Patients Undergoing Whole Brain Radiation Therapy for Brain Metastasis. New Jersey : Rutgers, The State University of New Jersey . Ryu J. K. Jantaratnotai N. Serrano-Perez M. C. McGeer P. L. McLarnon J. G. ( 2011 ). …

Bone targeted nano-drug and nano-delivery.

There are currently no targeted delivery systems to satisfactorily treat bone-related disorders. Many clinical drugs consisting of small organic molecules have a short circulation half-life and do not effectively reach the diseased tissue site. This coupled with repeatedly high dose usage that leads to severe side effects. With the advance in nanotechnology, drugs contained within a nano-delivery device or drugs aggregated into nanoparticles (nano-drugs) have shown promises in targeted drug delivery. The ability to design nanoparticles to target bone has attracted many researchers to develop n

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… | 199 MSNs_ZOL | DOX | Increased | 258 MSNs_ZOL | PL | Increased | 259 Ag2S_ALN | DOX | Increased | 260 PDA_ALN | SN38 | Increased | 261 RGD | Bortezomib | Increased | 262 Osteosarcoma | PEG | DOX | Increased | 263 Cu_MNSs | Cu, Si | Cell model only | 264 PLGA–nHAP | ZOL | Model | 265 iron oxide | Riluzole …

Opinion: more mouse models and more translation needed for ALS.

Amyotrophic lateral sclerosis is a complex disorder most of which is 'sporadic' of unknown origin but approximately 10% is familial, arising from single mutations in any of more than 30 genes. Thus, there are more than 30 familial ALS subtypes, with different, often unknown, molecular pathologies leading to a complex constellation of clinical phenotypes. We have mouse models for many genetic forms of the disorder, but these do not, on their own, necessarily show us the key pathological pathways at work in human patients. To date, we have no models for the 90% of ALS that is 'sporadic'. Potenti

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… Three treatments for ALS, riluzole, edaravone and AMX0035 are approved in different geographical areas but these drugs only prolong life by a few months in some patients and may not be appropriate for all individuals [ 3 ]. …

Нейрофильтрационная тяжелая цепочка в вторичном прогрессивном множественном склерозе.

Для отслеживания прогресса в испытаниях MS необходимы биомаркеры. Нейрофильтрационная тяжелая цепочка (NfH) используется недостаточно из-за ограничений на анализ. ЦЕЛЬ: Изучение дополнительной ценности церебрально-пинальной жидкости (CSF) NfH в вторичном прогрессивном множественном склерозе (SPMS) с использованием современных иммуномасс. Это исследовательское исследование было частью судебного процесса по делу MS-SMART. Клинические оценки (включая расширенную шкалу показателей инвалидности, функцию верхней и нижней частей конечностей, визуальную акумуляцию и проверку параметров символических з

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… The Multiple Sclerosis-Secondary Progressive Multi-Arm Randomization Trial (MS-SMART; NCT01910259 ) was a multi-arm, placebo-controlled trial investigating the neuroprotective role of amiloride, fluoxetine and riluzole in people with secondary progressive multiple sclerosis (SPMS). 20 – 22 The trial …

Oral Presentations

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Сфингосин 1-phosphate рецептор 1 Модераторы оказывают нейрозащитное воздействие на нарушения центральной нервной системы.

Фингозин 1-phosphate (S1P) Пути подачи сигналов имеют важные и разнообразные функции. Рецепторы S1P (S1PR) участвуют в регулировании торговли лимфоцитами, сердечно-церебральной функции, сосудистой проницаемости и бронхиолярного тона и были признаны в качестве терапевтических целей для различных заболеваний. Ряд лекарственных средств, связанных с траекторией подачи сигналов S1P, был утвержден для клинического использования при лечении множественных склерозов, и многие аналогичные препараты в настоящее время также проходят испытания в ходе клинических испытаний на различных этапах. Как представл

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… Riluzole was the first drug approved for the treatment of ALS, and although many new ALS drugs are already in phase II and phase III clinical trials, they all appear to have limited therapeutic efficacy at this time ( Xu et al., 2021 ). …

Colorectal Cancer at the Crossroads: The Good, the Bad, and the Future of Platinum-Based Drugs.

Colorectal cancer (CRC) remains a significant global health challenge, ranking third in incidence and second in mortality among cancers worldwide. This review addresses the complex landscape of CRC, focusing on incidence, mortality trends, preventive strategies, and the evolving therapeutic approaches, particularly highlighting the role of platinum-based drugs like oxaliplatin (OXP). It also underscores the increasing burden of CRC, with factors such as westernized diets, aging populations, and genetic predispositions contributing to its prevalence. Therapeutically, early detection greatly enh

Интеграция нанотехнологий в онкологию для передовых стратегий наночастиц в целевую диагностику и лечение рака.

Рак остается одной из основных глобальных проблем в области здравоохранения. Обычная терапия часто ограничивается низкой избирательностью опухолей, системной токсичностью, резистентностью к многочисленным лекарствам и неоптимальными фармакокинетиками. Нанотехнология предлагает преобразующий подход в онкологии. Она позволяет осуществлять целенаправленные поставки наркотиков, контролировать или стимулировать их высвобождение и использовать многофункциональные платформы, сочетающие в себе терапию и диагностику. Нанопчасти повышают растворимость наркотиков, продлевают циркуляцию и повышают внутрик

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… For neurodegenerative conditions, treatments include Riluzole NPs for amyotrophic lateral sclerosis [ 11 ], and Glatopa ® for multiple sclerosis [ 12 ]. Nanomedications such as DepoDur™ [ 13 ], and Exparel ® [ 14 ] have enhanced pain management. …

Dibromo-Edaravone Induces Anti-Erythroleukemia Effects via the JAK2-STAT3 Signaling Pathway.

Acute erythroid leukemia (AEL) is a rare and aggressive hematological malignancy managed with chemotherapy, targeted therapies, and stem cell transplantation. However, these treatments often suffer from limitations such as refractoriness, high toxicity, recurrence, and drug resistance, underscoring the urgent need for novel therapeutic approaches. Dibromo-edaravone (D-EDA) is a synthetic derivative of edaravone (EDA) with unreported anti-leukemic properties. In this study, D-EDA demonstrated potent cytotoxicity against HEL cells with an IC50 value of 8.17 ± 0.43 μM using an MTT assay. Morpholo

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… Riluzole and edaravone: A tale of two amyotrophic lateral sclerosis drugs. Med. Res. Rev. 2019;39:733–748. doi: 10.1002/med.21528. 9. Dang R., Wang M., Li X., Wang H., Liu L., Wu Q., Zhao J., Ji P., Zhong L., Licinio J., et al. …

Кинуреньенс и митохондриальные расстройства в многоразовом склерозе.

Множественный склероз (MS) — хроническое аутоиммунное заболевание, характеризующееся воспалением, обезвоживанием и нейродегенерацией в центральной нервной системе. Патогенез MS связан с иммунной атаки на миелин и нейроны, сопровождаемой дисфункцией мозга в крови и хроническим воспалением CNS. Центральное значение для патологии MS имеет дисрегулирование кинуреньинового пути, который метаболизирует триптофан в нейроактивные соединения. Активация Kynurenin Translation (KP) под воздействием подстрекательских цитокинов приводит к образованию как нейрозащитных (например, кинуриновой кислоты, КИНА),

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… Table 3 summarises six drugs that have been identified as promising candidates for further investigation in MS: ibudilast, riluzole, amiloride, pirfenidone, fluoxetine, and oxcarbazepine. …

Эффективность Куркумина в нейродегенеративных болезнях: от фармакокинетических барьеров до передовых систем доставки.

Предыстория и цели: Основные нейродегенеративные заболевания (НД) - болезнь Альцгеймера (AD), болезнь Паркинсона (PD), множественный склероз (MS) и амиотропический боковой склероз (ALS) - создают растущее бремя для здоровья людей во всем мире при отсутствии доступных методов лечения, позволяющих вести борьбу с заболеваниями. Куркумин, полифенол из Curcuma longa, является многообещающим кандидатом из-за его плейотропного антиоксиданта, антивоспалительного и нейрозащитного профиля, наблюдаемого главным образом в доклинических моделях, но плохой оральной биодоступности ().<1%) и незначительное пр

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… More recently, Ahmadi et al. published the first randomized, double-blind, placebo-controlled pilot clinical trial of nanocurcumin (80 mg/day) as an adjunct therapy to riluzole, in which nanocurcumin was associated with a reduced risk of the combined outcome of mortality or need for mechanical ventilation …

Recent Insights in Multi-Target Drugs in Pharmacology and Medicinal Chemistry.

Many of the drugs used in treatment today have been designed based on the "specificity paradigm". Resistance has developed against drugs designed using this approach, leading to a decrease in their effectiveness. In addition, it is well-documented in the literature that diseases with complex etiologies, such as Alzheimer's, Parkinson's, and cancer are influenced by multiple genetic and/or environmental factors. As a result, specificity paradigm is often insufficient for treating these diseases. Therefore, there is a need to develop drugs that interact with multiple targets simultaneously throu

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… [ 187 ] ALS ALS is a neurodegenerative disorder marked by the degeneration of lower and upper motor neurons, resulting in muscle atrophy, paralysis, and respiratory failure within 3–5 years postdiagnosis, ultimately culminating in the patient's death. [ 188 ] Edaravone, an excitotoxic agent, and Riluzole … intricate landscape. [ 191 ] The multifactorial and complex molecular causes of ALS suggest that polypharmacology may be a promising treatment approach. [ 192 ] Albertini et al. designed and synthesized a series of compounds that can interact with multiple targets by combining the pharmacophore groups of riluzole …

Pomalidomide mitigates neuronal loss, neuroinflammation, and behavioral impairments induced by traumatic brain injury in rat.

BACKGROUND: Traumatic brain injury (TBI) is a global health concern that typically causes emotional disturbances and cognitive dysfunction. Secondary pathologies following TBI may be associated with chronic neurodegenerative disorders and an enhanced likelihood of developing dementia-like disease in later life. There are currently no approved drugs for mitigating the acute or chronic effects of TBI. METHODS: The effects of the drug pomalidomide (Pom), an FDA-approved immunomodulatory agent, were evaluated in a rat model of moderate to severe TBI induced by controlled cortical impact. Post-TBI

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… Riluzole attenuates cortical lesion size, but not hippocampal neuronal loss, following traumatic brain injury in the rat. J Neurosci Res. 1998;52(3):342–9. doi: 10.1002/(SICI)1097-4547(19980501)52:3&#x0003c;342::AID-JNR10&#x0003e;3.0.CO;2-8. 30. Schmued LC, Hopkins KJ. …

Всеобъемлющий и систематический обзор по вопросу о добавке ресвератрола в качестве перспективного кандидата в отношении болезни сетчатки сетчатки: акцент на механизмах действий на основе доклинических исследований.

Resveratrol — естественный полифенолический соединение, демонстрирующее большой потенциал нейрозащиты, борьбы с воспалением и антиоксидацией. Предыдущие исследования показали, что ресвератрол может эффективно лечить различные животные модели болезней сетчатки. ПУРПОСЕ: Цель исследования состояла в том, чтобы использовать экспериментальную модель животных для оценки эффективности лечения заболеваний, связанных с сетчаткой, в рамках различных видов заболеваний, связанных с животным, таких, как ишемия-реперциозная травма, диабетическая ретинопатия, глаукома, хроническая окулярная гипертония, опти

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… Riluzole- and resveratrol-induced delay of retinal ganglion cell death in an experimental model of glaucoma. Curr. Eye Res. 41, 59–69. 10.3109/02713683.2015.1004719 Pisoschi A. M., Pop A. (2015). The role of antioxidants in the chemistry of oxidative stress: a review. Eur. J. Med. …

Multiple Facets of Autophagy and the Emerging Role of Alkylphosphocholines as Autophagy Modulators.

Autophagy is a highly conserved multistep process and functions as passage for degrading and recycling protein aggregates and defective organelles in eukaryotic cells. Based on the nature of these materials, their size and degradation rate, four types of autophagy have been described, i.e. chaperone mediated autophagy, microautophagy, macroautophagy, and selective autophagy. One of the major regulators of this process is mTOR, which inhibits the downstream pathway of autophagy following the activation of its complex 1 (mTORC1). Alkylphosphocholine (APC) derivatives represent a novel class of a

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… Study Design/Registry Number | Regimen | Indication/Autophagy Biomarker | Indication/Aims–Results/Status | Reference Phase II R, DB, PC, MC NCT03693781 Eudract n.2017-004459-21 | Colchicine 0.01 mg/kg/d; 0.005 mg/kg/d Riluzole: 100 mg/d Treatment: 30 wt Follow-up: 24w | ALS/Quantification of mRNA and … Two autophagy modulators, colchicine, which upregulates autophagy-related proteins in motor neurons in combination with riluzole ( Mandrioli et al., 2019 ), and the mTOR inhibitor rapamycin (sirolimus) ( Mandrioli et al., 2018 ) are being evaluated for their therapeutic efficacy against ALS in two separate …

Neurodegeneration: can metabolites from Eremurus persicus help?

The number of patients affected by neurodegenerative diseases is increasing worldwide, and no effective treatments have been developed yet. Although precision medicine could represent a powerful tool, it remains a challenge due to the high variability among patients. To identify molecules acting with innovative mechanisms of action, we performed a computational investigation using SAFAN technology, focusing specifically on HuD. This target belongs to the human embryonic lethal abnormal visual-like (ELAV) proteins and plays a key role in neuronal plasticity and differentiation. The results high

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… The treatments available in this field are often disease-specific and involve the use of small molecules, like memantine, carbidopa, or riluzole, or monoclonal antibodies, like aducanumab, but they are always associated with poor efficacy ( Lamptey et al., 2022 ). …

Novel Strategies for Cancer Combat: Drug Combination Using Repurposed Drugs Induces Synergistic Growth Inhibition of MCF-7 Breast and HT-29 Colon Cancer Cells.

Our group developed a new model of drug combination consisting of the use of antineoplastic drugs and different repurposed drugs, having demonstrated that antimalarial and central nervous system (CNS) drugs have a promising anticancer profile as standalone agents, as well as in combined regimens. Here, we evaluated the anticancer profiles of two different CNS drugs (edaravone and quetiapine), both alone and in combination with antineoplastic agents for breast and colon cancer, to explore whether these repurposed drugs could synergistically enhance the anticancer potential of chemotherapeutic d

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… Two Decades-Long Journey from Riluzole to Edaravone: Revisiting the Clinical Pharmacokinetics of the Only Two Amyotrophic Lateral Sclerosis Therapeutics. Clin. Pharmacokinet. 2018;57:1385–1398. doi: 10.1007/s40262-018-0655-4. 33. Ali Z.K., Baker D.E. Formulary Drug Review: Edaravone. Hosp. …

The Role of Nucleotide Excision Repair in Cisplatin-Induced Peripheral Neuropathy: Mechanism, Prevention, and Treatment.

Platinum-based chemotherapy-induced peripheral neuropathy (CIPN) is one of the most common dose-limiting effects of cancer treatment and results in dose reduction and discontinuation of life-saving chemotherapy. Its debilitating effects are often permanent and lead to lifelong impairment of quality of life in cancer patients. While the mechanisms underlying the toxicity are not yet fully defined, dorsal root ganglia sensory neurons play an integral role in symptom development. DNA-platinum adducts accumulate in these cells and inhibit normal cellular function. Nucleotide excision repair (NER)

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… Targeting the TREK-1 potassium channel via riluzole to eliminate the neuropathic and depressive-like effects of oxaliplatin. Neuropharmacology. 2018;140:43–61. doi: 10.1016/j.neuropharm.2018.07.026. 30. Ozkan K., Ertas H., Caner B. Platinum-induced neurotoxicity: A review of possible mechanisms. …

Insights into platinum-induced peripheral neuropathy-current perspective.

Cancer is a global health problem that is often successfully addressed by therapy, with cancer survivors increasing in numbers and living longer world around. Although new cancer treatment options are continuously explored, platinum based chemotherapy agents remain in use due to their efficiency and availability. Unfortunately, all cancer therapies affect normal tissues as well as cancer, and more than 40 specific side effects of platinum based drugs documented so far decrease the quality of life of cancer survivors. Chemotherapy-induced peripheral neuropathy is a frequent side effects of plat

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… Targeting the TREK-1 potassium channel via riluzole to eliminate the neuropathic and depressive-like effects of oxaliplatin. Neuropharmacology. 2018;140:43–61. doi: 10.1016/j.neuropharm.2018.07.026. 72. Prakash A, Doublie S. Base excision repair in the mitochondria. …

Exploration and Development of PPAR Modulators in Health and Disease: An Update of Clinical Evidence.

Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that govern the expression of genes responsible for energy metabolism, cellular development, and differentiation. Their crucial biological roles dictate the significance of PPAR-targeting synthetic ligands in medical research and drug discovery. Clinical implications of PPAR agonists span across a wide range of health conditions, including metabolic diseases, chronic inflammatory diseases, infections, autoimmune diseases, neurological and psychiatric disorders, and malignancies. In this review we aim to consolidate exist

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… Dupuis et al. (2012) reported no improvement upon co-administration of 45 mg/day of pioglitazone and 100 mg/day of riluzole when compared to a placebo group, with increased patient death (30:24 by the end of two years) and a hazard ratio of 1.21 at the end of the trial [ 237 ]. … In another Phase I/II clinical trial, co-administration of riluzole, tretinoin, and pioglitazone did not delay the disease progression of ALS [ 238 ]. Existing clinical evidence does not support the use of pioglitazone in ALS treatment. …